Depsipeptides containing non-natural amino acids

摘要

A depsipeptide containing a non-natural amino acid(s) having the formula (1) wherein R<1> represents a C5-C20 alkyl group and others; R<2> represents -O-CO-CH(R<5>)-X-CH(R<6>)-NH- (wherein X represents N(R<7>)-CO, CH2-CO, CH2-CH2 and others, R<5>, R<6>, and R<7> represent a hydrogen atom or a C1-C6 alkyl group); R<3> represents (wherein Y represents N(R<12>)-CO, N(R<13>)-CH2, CH2-CO, CH2-CH2 and others, n represents an integer of 1-3, R<9>, R<10>, R<12> and R<13> represent a hydrogen atom or a straight or branched C1-C6 alkyl group and R<11> represents a protecting group for an amine); R<4> represents a hydroxyl group, a straight or branched C1-C6 alkoxy group, a benzyloxy group, A, A-B or -NH-CH(R<14>)-Z-CH(R<15>)-COR<16> (wherein Z represents CH2-N(R<17>), CO-CH2, CO-N(R<18>), CH2-CH2 and others, R<14>, R<15>, R<17> and R<18> represent a hydrogen atom or a straight or branched C1-C6 alkyl group, R<16> represents a hydroxyl group, a straight or branched C1-C6 alkoxy group or a benzyloxy group); and A and B represent an amino acid residue or an N-methyl derivative thereof. The above depsipeptides have a promoting activity on the production of apolipoprotein E, and are useful as a therapeutic agent for neurologic damages, especially dementia, and hyperlipemia.